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首页> 外文期刊>Journal of Microencapsulation: Microcapsules Liposomes Nanoparticles Microcells Microspheres >Poly (epsilon-caprolactone) nanocapsules for oral delivery of raloxifene: process optimization by hybrid design approach, in vitro and in vivo evaluation
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Poly (epsilon-caprolactone) nanocapsules for oral delivery of raloxifene: process optimization by hybrid design approach, in vitro and in vivo evaluation

机译：用于口服递送雷洛昔芬的聚（ε-己内酯）纳米胶囊：通过混合设计方法进行工艺优化，体外和体内评估

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摘要

Raloxifene HCl (RLX), a selective oestrogen receptor modulator, has low oral bioavailability (<2%) in humans due to its poor aqueous solubility and extensive first-pass metabolism in gut. In this study, we optimised the method of preparation for poly (epsilon-caprolactone) (PCL) based nanocapsules of RLX by double emulsion method (w/o/w). A hybrid design approach, Plackett-Burman design followed by rotatable central composite design, was used to arrive at the optimised formulation. The optimised formulation was subjected to in vitro and in vivo evaluation. RLX loaded nanocapsules were spherical in shape with particle size less than 200nm and high encapsulation efficiency (>80%). RLX-loaded nanocapsules showed 2.1-fold increase in oral bioavailability compared to free RLX. IV pharmacokinetic studies indicated that RLX loaded into nanocapsule had significantly low clearance in comparison with free RLX. Designed nanocapsules showed promise as delivery systems to enhance oral bioavailability and in reducing clearance of raloxifene.
机译：盐酸雷洛昔芬（RLX）是一种选择性雌激素受体调节剂，由于其水溶性差和在肠道中广泛的首过代谢，因此在人体内的口服生物利用度较低（<2％）。在这项研究中，我们优化了通过双乳液法（w / o / w）制备聚（ε-己内酯）（PCL）基RLX纳米胶囊的方法。使用混合设计方法（Plackett-Burman设计，然后是可旋转的中央复合设计）来获得优化的配方。对优化的制剂进行体外和体内评估。载有RLX的纳米胶囊呈球形，粒径小于200nm，并且包封效率高（> 80％）。与游离RLX相比，负载RLX的纳米胶囊的口服生物利用度提高了2.1倍。 IV药代动力学研究表明，与游离RLX相比，装入纳米胶囊的RLX的清除率明显较低。设计的纳米胶囊显示出有望作为增强口服生物利用度并减少雷洛昔芬清除率的递送系统。

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